(1) Field of the Invention
The present invention relates to chemotherapeutic tripeptide compounds consisting of dichlorodiethylaminophenylalanine, parafluorophenylalanine, and methionine covalently linked which are useful in the treatment of tumor cells. The present invention also relates to a process for preparation and to a process for administration of the chemotherapeutic compounds.
The present invention also provides pharmaceutical compositions which contain at least one of the new tripeptide compounds in admixture with a solid or liquid pharmaceutical carrier that is physiologically acceptable.
The present invention then relates to chemotherapy against tumor of animals by administering the various chemotherapeutic compounds to test animals by intravenous or intraperitoneal or by oral route.
(2) Prior Art
Chemotherapy as been and still is an object of intense research. Certain positive results have undoubtedly been achieved, especially by means of polychemotherapy realized by associating different active substances according to carefully developed protocols. However, the ideal therapy has not been found. The need to find new active substances has been particularly emphasized. All the foregoing justifies continuous research directed toward preparing new chemotherapeutic compounds active against cancerous tumors. There are already known peptides having anti-tumor activity, consisting of both normal and antimetabolic amino acids, coupled by means of a peptide bond. Such peptides have for years been in therapeutic use with favorable results both in monochemotherapy and in polychemotherapy.
The amino acid dichlorodiethylaminophenylalanine which contains the --N(CH.sub.2 CH.sub.2 Cl).sub.2 group in the meta-position of the benzene ring displays for certain tumors greater activity than the para-compound. The highly active ortho-derivative is the least stable and the most toxic of the three isomers.